Expanding the scope of synthetic 1,2,4-trioxanes towards Trypanosoma cruzi and Leishmania donovani

被引：5
作者：
Medran, Noelia S. [1 ,2 ]
Saye, Melisa [3 ,4 ]
Pereira, Claudio A. [3 ,4 ]
Tekwani, Babu L. [5 ,6 ,7 ]
La-Venia, Agustina [1 ,2 ]
Labadie, Guillermo R. [1 ,2 ]
机构：
[1] Univ Nacl Rosario, Inst Quim Rosario IQUIR, CONICET, Suipacha 531,S2002LRK, Rosario, Argentina
[2] Univ Nacl Rosario, Fac Ciencias Bioquim & Farmaceut, Dept Quim Organ, Rosario, Argentina
[3] Univ Buenos Aires, Fac Med, Inst Invest Med A Lanari, Buenos Aires, DF, Argentina
[4] Univ Buenos Aires, Inst Invest Med IDIM, Lab Parasitol Mol, Consejo Nacl Invest Cient & Tecn, Buenos Aires, DF, Argentina
[5] Univ Mississippi, Sch Pharm, Natl Ctr Nat Prod Res, University, MS 38677 USA
[6] Univ Mississippi, Sch Pharm, Dept Pharmacol, University, MS 38677 USA
[7] Southern Res, Dept Infect Dis, Div Drug Discovery, Birmingham, AL 35205 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2020年 / 30卷 / 20期
基金：
英国科研创新办公室;
关键词：
Artemisinin; Trioxanes; Trypanosoma cruzi; Leishmania donovani; Tropical neglected diseases; IN-VITRO; BRUCEI-RHODESIENSE; MEDICINAL-PLANTS; ARTEMISININ; DERIVATIVES; SUSCEPTIBILITY; ARTESUNATE; DISCOVERY; EFFICACY; THERAPY;
D O I：
10.1016/j.bmcl.2020.127491
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of synthetic 1,2,4-trioxanes related to artemisinin was tested against L. donovani and T. cruzi parasites. This screening identified some active compounds, with key common structural features. Interestingly, these selected trioxanes were efficient against both parasites, and achieved antiparasitic activities comparable or superior than those presented by the corresponding reference drugs, artemisinin and artesunate. This study represents the first example of synthetic trioxanes evaluated on T. cruzi and provides possible candidates for developing new drugs for the treatment of leishmaniasis and Chagas disease.
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页数：5
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